Trametinib

Trametinib

Clinical data
Trade names	Mekinist
Pregnancy category	US: D (Evidence of risk)
ATC code	L01XE25 (WHO)
Legal status
Legal status	US: ℞-only
Identifiers
IUPAC name N-(3-{3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)acetamide
Synonyms	GSK1120212
CAS Number	871700-17-3
PubChem CID	11707110
ChemSpider	9881833
UNII	33E86K87QN
ChEBI	CHEBI:75998
ChEMBL	CHEMBL2103875
ECHA InfoCard	100.158.135
Chemical and physical data
Formula	C26H23FIN5O4
Molar mass	615.39 g/mol
3D model (Jmol)	Interactive image
SMILES Ic1ccc(c(F)c1)N\C3=C\2/C(=O)N(C(=O)N(C/2=C(\C(=O)N3C)C)c4cccc(NC(=O)C)c4)C5CC5
InChI InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34) Key:LIRYPHYGHXZJBZ-UHFFFAOYSA-N

Trametinib (trade name Mekinist) is a cancer drug. It is a MEK inhibitor drug with anti-cancer activity.

It inhibits MEK1 and MEK2.

Trametinib had good results for metastatic melanoma carrying the BRAF V600E mutation in a phase III clinical trial. In this mutation, the amino acid valine (V) at position 600 within the BRAF gene has become replaced by glutamic acid (E) making the mutant BRAF gene constitutively active.

In May 2013, trametinib was approved as a single-agent by the Food and Drug Administration for the treatment of patients with V600E mutated metastatic melanoma. Clinical trial data demonstrated that resistance to single-agent trametinib often occurs within 6 to 7 months. To overcome this, trametinib was combined with the BRAF inhibitor dabrafenib. As a result of this research, on January 8, 2014, the FDA approved the combination of dabrafenib and trametinib for the treatment of patients with BRAF V600E/K-mutant metastatic melanoma.